Identification of cytotoxic, T-cell-selective 1,4-benzodiazepine-2,5-diones

Francis, Tasha M.; Sundberg, Thomas B.; Groendyke, Todd M.; Opipari, Anthony W.; Glick, Gary D.

doi:10.1016/j.bmcl.2006.01.113

Cited by 11 publications

(3 citation statements)

References 14 publications

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“…Phenotype screening of Ramos B cells revealed that Bz-423 caused cell shrinkage, nuclear condensation, cytoplasmic vacuolization, membrane blebbing, and DNA fragmentation. Other 1,4-benzodiazepine derivatives were found to selectively target T cells ( Francis et al, 2006 ; Gatza et al, 2011 ; Wahl et al, 2012 ; Tkachev et al, 2015 ). Bz-423 did not strongly bind to the peripheral benzodiazepine receptor.…”

Section: Bz-423 Binds To Oscp Of Mitochondrial F O mentioning

confidence: 99%

Visualizing Mitochondrial FoF1-ATP Synthase as the Target of the Immunomodulatory Drug Bz-423

2018

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Targeting the mitochondrial enzyme FoF1-ATP synthase and modulating its catalytic activities with small molecules is a promising new approach for treatment of autoimmune diseases. The immunomodulatory compound Bz-423 is such a drug that binds to subunit OSCP of the mitochondrial FoF1-ATP synthase and induces apoptosis via increased reactive oxygen production in coupled, actively respiring mitochondria. Here, we review the experimental progress to reveal the binding of Bz-423 to the mitochondrial target and discuss how subunit rotation of FoF1-ATP synthase is affected by Bz-423. Briefly, we report how Förster resonance energy transfer can be employed to colocalize the enzyme and the fluorescently tagged Bz-423 within the mitochondria of living cells with nanometer resolution.

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Section: Bz-423 Binds To Oscp Of Mitochondrial F O mentioning

confidence: 99%

Visualizing Mitochondrial FoF1-ATP Synthase as the Target of the Immunomodulatory Drug Bz-423

2018

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“…Benzodiazepine derivatives are important compounds family with various biological properties. They have attributed to many pharmacological activities among which are tranquilisant, antiviral, anti-inflammatory, analgesic, antipyretic and anticonvulsivant [1][2][3][4][5][6][7][8][9][10][11][12]. Benzodiazepine adducts are also considered as important precursors in the synthesis of benzimidazole, pyrazole, isoxazole and quinoxaline derivatives [13][14][15][16][17][18].…”

Section: Introductionmentioning

confidence: 99%

A Convenient Method for the Synthesis of 1,5-benzodiazepin-2-one

Rida¹,

Meslouhi²,

Ahabchane³

et al. 2008

TOOCJ

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New 3-hydroxy-1,5-benzodiazepin-2-ones were synthesized through condensation between ophenylenediamines with glycidic ester. Alkylation and oxidation of some of the obtained compounds were also explored in different conditions yielding various oxidized and alkylated benzodiazepines. The structural elucidation of the synthesized compounds was achieved by MS, NMR spectroscopy and also through X-ray diffraction analysis. The glycidic ester was thus shown to be an interesting synthon in the synthesis of new 1,5-benzodiazepines used in alkylation and oxidation reactions.

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“…They have attributed to many pharmacological activities among which are tranquilisant, antiviral, anti-inflammatory, analgesic, antipyretic and anticonvulsivant [1][2][3][4][5][6][7][8][9][10][11][12]. Benzodiazepine adducts are also considered as important precursors in the synthesis of benzimidazole, pyrazole, isoxazole and quinoxaline derivatives [13][14][15][16][17][18].…”

Section: Introductionmentioning

confidence: 99%